BET bromodomain inhibitor 1 is an orally active and selective inhibitor of bromodomain and extra-terminal (BET) bromodomains. It demonstrates anti-cancer activity by inducing G1-phase cell cycle arrest, inhibiting c-Myc expression, and upregulating p21 levels. Its primary applications involve research into acute myeloid leukemia, acute leukemia, and multiple myeloma.
- Orally active and selective BET bromodomain inhibitor.
- High affinity for BRD4 (IC50: 2.6 nM) and other BET bromodomains.
- Demonstrates anti-cancer activity by inducing G1-phase cell cycle arrest.
- Effective against various cancer cell lines (Kasumi 1, MM1.S, MV4-11, and RS4-11).
- Excellent selectivity for BET bromodomain family over other bromodomains.
- Does not inhibit five cytochrome P450 enzymes.
- Exhibits strong antitumor activities in in-vivo models.